BRD5075
Based on 1 Customer Validation
BRD5075 is a selective GPR65 activator. BRD5075 enhances GPR65 activity under acidic conditions, promotes Gαs-dependent signaling pathways, including cAMP production and G protein recruitment. BRD5075 regulates the cytokine and chemokine expression network in dendritic cells, and inhibits the expression of pro-inflammatory cytokines and chemokines in a GPR65-dependent manner. BRD5075 is applicable to research related to inflammatory bowel disease.
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- Purity: 98.08%
- 화학식: C23H23N5O3
- 분자량:417.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
BRD5075 (1.56-50 μM; 30 min) potently and specifically induces cAMP production in HeLa cells via positive allosteric modulation of wild-type hGPR65 and mGPR65, with no activity against the related pH-sensing receptors hGPR4 or hGPR68[1].
BRD5075 (5-20 μM; 3 hours) inhibits LPS (HY-D1056)-induced TNF secretion in human MDDCs under pH 6.6 conditions[1].
BRD5075 (1.56-50 μM; 72 hours) shows no cytotoxicity against hGPR65-expressing HeLa cells at concentrations up to 25 μM, and only exhibits extremely low cytotoxicity at 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells stably expressing wild-type hGPR65
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Concentration:1.56, 3.125, 6.25, 12.5, 25 and 50 μM
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Incubation Time:72 hours
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Result:Was not cytotoxic to hGPR65-expressing HeLa cells over 72 hours, with only a slight decrease in cell viability observed at 50 μM.
Chemical Information
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Appearance Solid
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분자량 417.46
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화학식 C23H23N5O3
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Color Off-white to light yellow
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SMILES
O=C1C=C(C2=CC=C(COC(C)C)C=C2)NC3=C(C(NC4=NC=C(C)C=C4)=O)C=NN31
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (239.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | 59.8860 mL |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | 11.9772 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 mL | 5.9886 mL | |
| 15 mM | 0.1597 mL | 0.7985 mL | 1.5970 mL | 3.9924 mL | |
| 20 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9943 mL | |
| 25 mM | 0.0958 mL | 0.4791 mL | 0.9582 mL | 2.3954 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7985 mL | 1.9962 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4971 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4791 mL | 1.1977 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9981 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7486 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5989 mL |
BRD5075 Related Classifications
HY-162734 Related Classifications
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